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Bioorg Med Chem Lett. 2012 Jan 1;22(1):613-8. doi: 10.1016/j.bmcl.2011.10.071. Epub 2011 Nov 3.

Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.

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  • 1Merck Research Laboratories, MSD, PO Box 20, 5340 BH Oss, The Netherlands.

Abstract

Optimization of our previously described pyrrolopiperidone series led to the identification of a new benzamide sub-series, which exhibits consistently high potency in biochemical and cell-based assays throughout the series. Strong inhibition of LPS-induced production of the cytokine TNFα is coupled to the regulation of HSP27 phosphorylation, indicating that the observed cellular effects result from the inhibition of MK2. X-ray crystallographic and computational analyses provide a rationale for the high potency of the series.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
22119462
[PubMed - indexed for MEDLINE]
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